[CAS NO. 1140517-08-3] ML604440
PRODUCTS SPECIFICATIONS [1140517-08-3]
DESCRIPTION [1140517-08-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 388.19 |
| Molecular Formula | C17H24BF3N2O4 |
| SMILES | CC(C)C[C@@H](B(O)O)NC(C(NC(C1=CC=CC=C1C(F)(F)F)=O)(C)C)=O |
2 Publications Citing Use of MCE
Summary
ML604440 is a specific and cell-permeable Proteasome β1i ( LMP2 ) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor [1] [2] [3] .
IC50 & Target
proteasome β1i (LMP2) subunit inhibitor [1]
In Vitro
ML604440 (300 nM; overnight) treatment shows no influence on the surface expression of H-2K
b
in wt or LMP7-deficient mice splenocytes
[2]
.
ML604440 (300 nM; 24 h) treatment shows no significant inhibition of IL-6 secretion by mouse splenocytes or human PBMCs
[2]
.
ML604440 (300 nM; 3 d) shows no influence on the percentage of IL-17A-producing CD4
+
T cells
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ML604440 (intraperitoneal injection; 10 mg/kg; once daily; 7 d) treatment inhibits LMP2 in vivo, shows no significant changes in platelet counts [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male C57BL/6J mice (6-8-wks old) injected with anti-platelet monoclonal antibody [3] |
| Dosage: | 10 mg/kg |
| Administration: | Intraperitoneal injection; 10 mg/kg; once daily; 7 days |
| Result: |
Inhibited LMP2 in vivo.
Showed no significant improvement in platelet counts in mice immunized by monoclonal rat anti-mouse CD41 platelet antibody. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 257.61 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5761 mL | 12.8803 mL | 25.7606 mL |
| 5 mM | 0.5152 mL | 2.5761 mL | 5.1521 mL |
| 10 mM | 0.2576 mL | 1.2880 mL | 2.5761 mL |
References
- [1] de Bruin G, et al. Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. J Med Chem. 2014 Jul 24;57(14):6197-209
- [2] Basler M, et al. Co-inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity. EMBO Rep. 2018 Dec;19(12). pii: e46512.
- [3] Sheng-Hong Du, et al. Co-Inhibition of the Immunoproteasome Subunits LMP2 and LMP7 Ameliorates Immune Thrombocytopenia. Front Immunol. 2021 Jan 20;11:603278.